SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD.
性状
Solid
IC50 & Target[1][2]
IC50: 44 nM (Human p38α)
体外研究(In Vitro)
SB 239063 (0.1–10 μM ; 29 hours, 47 hours) increases apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards.
SB 239063 potently inhibits IL-1 and TNF- a production in LPS-stimulated human peripheral blood monocytes with IC50 values of 120 nM and 350 nM, respectively.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Apoptosis Analysis
Cell Line:
Eosinophils (guinea pig BALs)
Concentration:
0.1μM, 1μM, 10μM
Incubation Time:
29 hours, 47 hours
Result:
Increased apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards.
体内研究(In Vivo)
SB 239063 (12 mg/kg; p.o.; 1 hour before and 4 hours after OA challenge; b.i.d. for 3 days) significantly inhibits the resultant antigen-induced airway eosinophilia.
SB 239063 (12 mg/kg; p.o.) almost abolishes ovalbumin (OA)-induced airway eosinophilia (~ 93% inhibition) by inhalation.
SB 239063 is a potent inhibitor of LPS-induced TNF-alpha production in the mouse peritoneal cavity with an EC50 of 5.8 mg/kg (2.8–10.3; 95% CL).
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male BALB/c mice (18–20 g)
Dosage:
12 mg/kg
Administration:
Oral administration; 1 h before and 4 h after OA challenge; bis in die for 3 days
Result:
Significantly inhibited the resultant antigen-induced airway eosinophilia.